Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 45, Issue 8, Pages 3480-3489Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2010.05.015
Keywords
Anacardic acids; Isobenzofuranones; Phthalides; Cytotoxicity screening
Categories
Funding
- CNPq
- FUNCAP
- FINEP [CTINFRA 970/2001, 1040091/2004, 01.04.0091.00]
- Universidade de Brasilia
- Universidade Federal do Ceara
- Universidade Catolica de Brasilia
- CAPES
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This work is part of a large program, which seeks to discover new antitumor isobenfuranones designed from anacardic acids. The synthetic strategy for the construction of the title compounds takes into consideration the use of inexpensive anacardic acids (2), the major natural cashew (Anacardium occidentale) nut-shell phenolic lipid, and features one-pot construction of fused-ring aromatic gamma-lactones, phthalides. The cytotoxicity screening in different human cancer cell lines (HL-60 leukemia, SF295 glioblastoma and MDA-MB435 melanoma) by the KIT assay showed that acyclic precursor (6), and isobenfuranones (1a and 1b) are active compounds. Interestingly, la exhibits significant antiproliferative effect against HL-60 cells and moderate activity against SF295 and MDA-MB435 cell lines. Analysis of mechanisms involved in the cytotoxic activity showed that active compounds were leading to DNA damage, triggering apoptosis or necrosis induction. (C) 2010 Elsevier Masson SAS. All rights reserved.
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